GNE 617
GNE 617 Basic information
- Product Name:
- GNE 617
- Synonyms:
-
- GNE 617
- GNE617
- GNE-617
- N-[[4-[(3,5-Difluorophenyl)sulfonyl]phenyl]methyl]imidazo[1,2-a]pyridine-6-carboxamide
- N-(4-((3,5-difluorophenyl)sulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carboxamide
- CS-1587
- GNE617;GNE 617
- Imidazo[1,2-a]pyridine-6-carboxamide, N-[[4-[(3,5-difluorophenyl)sulfonyl]phenyl]methyl]-
- CAS:
- 1362154-70-8
- MF:
- C21H15F2N3O3S
- MW:
- 427.42
- Product Categories:
-
- API
- Mol File:
- 1362154-70-8.mol
GNE 617 Chemical Properties
- Density
- 1.42±0.1 g/cm3(Predicted)
- solubility
- DMF:20.0(Max Conc. mg/mL);46.79(Max Conc. mM)
DMSO:78.67(Max Conc. mg/mL);26.22(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.47(Max Conc. mM) - pka
- 11.69±0.46(Predicted)
- form
- Powder
- color
- White to off-white
GNE 617 Usage And Synthesis
Uses
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
in vivo
In rats, GNE-617 (administered QD) and GNE-875 (administered BID) are associated with more severe retinal toxicity at similar exposures and dosing duration compared with GMX-1778 (administered BID). The mouse efficacy studies using GNE-617, GNE-618, and GMX-1778 are designed to assess efficacy and opportunistically used to assess retinal toxicity in mice. NAMPTi retinal toxicity is observed with GNE-617 and GMX-1778; however, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity[2].
References
[1] Shames DS, et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23. DOI:10.1158/1078-0432.CCR-13-1186
[2] Zabka TS, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72. DOI:10.1093/toxsci/kfu268
GNE 617Supplier
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- sales@boylechem.com
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